Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation.

Felts AS, Rodriguez AL, Blobaum AL, Morrison RD, Bates BS, Thompson Gray A, Rook JM, Tantawy MN, Byers FW, Chang S, Venable DF, Luscombe VB, Tamagnan GD, Niswender CM, Daniels JS, Jones CK, Conn PJ, Lindsley CW, Emmitte KA
J Med Chem. 2017 60 (12): 5072-5085

PMID: 28530802 · PMCID: PMC5484149 · DOI:10.1021/acs.jmedchem.7b00410

MeSH Terms (16)

Allosteric Regulation Aminopyridines Animals Chemistry Techniques, Synthetic Drug Evaluation, Preclinical HEK293 Cells High-Throughput Screening Assays Humans Macaca fascicularis Male Mice, Inbred Strains Picolinic Acids Rats, Sprague-Dawley Receptor, Metabotropic Glutamate 5 Structure-Activity Relationship Tissue Distribution

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